General description

A cell-permeable, pyrrolidine small molecule that promotes single human embryonic stem cell survival up to 20-fold over background (EC₅₀ = 3.9 M), with equal or higher potency than Y-27632 in 5 cell lines (SA461, SA181, SA167, SA121 and SA002) tested at 10 M. An in vitro high-content screening assay, which profiles a panel of more than 70 protein kinases, indicates that this small molecule is more selective than Y-27632 and only displays an inhibitory effect toward ROCK2 (>83% inhibition, ROCK1 was not included in the panel) and PRK2 (76% inhibition) at 10 M. Furthermore, it exhibits less cytotoxicity at a greater concentration of 30 M than Y-27632 without marked adverse effects for up to 120 hours.

A cell-permeable, pyrrolidine small molecule that promotes single human embryonic stem cell survival up to 20-fold over background (EC₅₀ = 3.9 M), with equal or higher potency than Y-27632 (Cat. No. 688000) in 5 cell lines (SA461, SA181, SA167, SA121 and SA002) tested at 10 M. An in vitro high-content screening assay, which profiles a panel of more than 70 protein kinases, indicates that this small molecule is more selective than Y-27632 and only displays an inhibitory effect toward ROCK2 (>83% inhibition, ROCK1 was not included in the panel) and PRK2 (76% inhibition) at 10 M. Furthermore, it exhibits less cytotoxicity at a greater concentration of 30 M than Y-27632 without marked adverse effects for up to 120 hours.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Andrews, P.D., et al. 2010. Biochem. J.432, 21.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)